Nanostructured lipid carriers (NLC) based topical gel of flurbiprofen: Design, characterization and in vivo evaluation

氟比洛芬 渗透 触变性 体内 色谱法 化学 红斑 Zeta电位 透皮 药代动力学 药理学 材料科学 医学 皮肤病科 纳米颗粒 纳米技术 生物化学 生物技术 复合材料 生物
作者
Fei Han,Ran Yin,Xin Che,Jing Yuan,Yanan Cui,He Yin,Sanming Li
出处
期刊:International Journal of Pharmaceutics [Elsevier BV]
卷期号:439 (1-2): 349-357 被引量:104
标识
DOI:10.1016/j.ijpharm.2012.08.040
摘要

Nanostructured lipid carriers (NLC)-based gel was developed as potential topical system for flurbiprofen (FP) topical delivery. The characterizations of the prepared semisolid formulation for topical application on skin were assessed by means of particle size distribution, zeta potential analysis, X-ray analysis, in vitro percutaneous penetration, rheological study, skin irritation test, in vivo pharmacodynamic evaluation and in vivo pharmacokinetic study. The NLC remained within the colloidal range and it was uniformly dispersed after suitably gelled by carbopol preparation. It was indicated in vitro permeation studies through rat skin that FP-NLC-gel had a more pronounced permeation profile compared with that of FP-loaded common gel. Pseudoplastic flows with thixotropy were obtained for all NLC-gels after storage at three different temperatures. No oedema and erythema were observed after administration of FP-NLC-gel on the rabbit skin, and the ovalbumin induced rat paw edema could be inhibited by the gel. The maximum concentration in plasma was 29.44 μg/ml and 2.49 μg/ml after oral and topical administration, respectively. While the amount of drug accumulated in skin after topical application was much higher than oral application. In conclusion, NLC-based gel could be a promising vehicle for topical delivery of FP.
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